TABLE 1.
Mutant hEAG1 channels with altered response to ICA
| Mutation in hEAG1 | Mean IC50 for ICA ± S.E.M. | n | Fold increase or decrease (↓) in IC50 |
|---|---|---|---|
| µM | |||
| (WT) | 0.44 ±0.03 | 5 | – |
| V356A** | 0.08 ±0.009 | 3 | 5.5 ↓ |
| V356E** | 28.8 ±2.6 | 3 | 65 |
| F359A* | 29.6 ±9.0 | 3 | 67 |
| F359L | >30 | 4 | >68 |
| L427A** | 0.17 ±0.01 | 3 | 2.6 ↓ |
| M431A* | 1.9 ±0.34 | 5 | 4.3 |
| L434A** | 8.5 ±0.08 | 5 | 19 |
| L434C** | 4.8 ±0.2 | 3 | 11 |
| M457A | >30 | 4 | >68 |
| M458A** | 20.2 ±1.2b | 4 | 46 |
| M458Ea | 0.45 ±0.08 | 3 | no change |
| L462A** | 0.05 ±0.005 | 3 | 8.6 ↓ |
| L463A** | 41.2 ±8.2b | 3 | 94 |
| Y464A** | 0.07 ±0.014 | 3 | 6.3 ↓ |
| I467A** | 1.1 ±0.05 | 3 | 2.5 |
| I467E** | 24.8 ±4.1b | 3 | 56 |
| F468A** | 3.1 ±0.48 | 4 | 7 |
hEAG1, human ether-a-go-go type 1; ICA, -nitro-N-(4-phenoxyphenyl)-benzamide (ICA-105574); WT, wild-type.
a
NS, nonsignificant (P > 0.05).
b
Effective IC50.
*
P < 0.01.
**
P < 0.001 compared with WT.